Welcome to Shanghai Probechem Biochemicals Co Ltd !Global Supplier of Chemical Probes, Inhibitors & Agonists.
Chemical Structure : M5049
CAS No.: 2101938-42-3
Catalog No.: PC-72049Not For Human Use, Lab Use Only.
M5049 (Enpatoran, M-5049) is a novel potent, selective TLR7/8 inhibitor with IC50 of 11.1/24.1 nM in HEK NF-kB-luciferase reporter cells assay, repectively
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 5 mg | $198 | In stock | |
| 10 mg | $298 | In stock | |
| 25 mg | $458 | In stock | |
| 50 mg | Get quote | ||
| 100 mg | Get quote |
Bulk size, bulk discount!
E-mail: sales@probechem.com
Tech Support: tech@probechem.com
M5049 (Enpatoran, M-5049) is a novel potent, selective TLR7/8 inhibitor with IC50 of 11.1/24.1 nM in HEK NF-kB-luciferase reporter cells assay, repectively.
M5049 (Enpatoran) is potent against TLR7 and TLR8 in PBMCs (IL-6 IC50=68.3 and 620 nM) as well as whole blood (IL-6 IC50=2.2 nM).
M5049 (Enpatoran) showed good selectivity and were found to be inactive against TLR3,TLR4 and TLR9 in vitro and in vivo, as wll as against a panel of 389 kinases as off-target profiling and at 1 mM M5049 only inhibited the activity of one kinase more than 50% (CAMKK2)
M5049 (Enpatoran) blocks multiple TLR7/8 RNA ligands. Treatment of BXSB-Yaa mice with M5049 (Enpatoran) led to an improvement in survival and reduction in kidney disease as evidenced by lower proteinuria.
| M.Wt | 320.319 | |
| Formula | C16H15F3N4 | |
| Appearance | Solid | |
| Storage |
|
|
| Solubility |
50 mM in DMSO (16.1 mg/mL) (Ultrasonic needed) |
|
| Chemical Name/SMILES |
8-Quinolinecarbonitrile, 5-[(3R,5S)-3-amino-5-(trifluoromethyl)-1-piperidinyl]- |
|
1. Vlach J, et al. J Pharmacol Exp Ther. 2021 Mar;376(3):397-409.
2. Port A, et al. Pharmacol Res Perspect. 2021 Oct;9(5):e00842.
Copyright © 2022 probechem.com. All Rights Reserved. probechem Copyright
